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Andosterone derivatives that inhibit AP-1 DNA binding and airway smooth muscle proliferation

机译:抑制AP-1 DNA结合和气道平滑肌增生的雄激素衍生物

摘要

There is described a method for the use of the adrenal steroid dehydroepiandrosterone and certain of its analogs to reduce growth of immortalized and malignant cell lines, according to the following formula: CHEM and CHEM wherein X is halogen, hydroxy, hydrogen, lower alkyl or lower alkoxy; Y is hydrogen or hydroxy; Z is lower alkyl or hydrogen. Dehydroepiandrosterone and its potent analogs 16 alpha -bromo-5-andtosten-17-one, 16 beta -bromo-5-androsten-17-one, 16 alpha -fluoro-5-androsten-17-one, 16 beta -fluoro-5-androsten-17-one, 16 alpha -bromo-5-androstan-17-one, 16 beta -bromo-5-androstan-17-one, 16 alpha -fluoro-5-androstan-17-one and 16 beta -fluoro-5-androstan-17-one impair activation of secondary growth response genes, and thus prove useful for the preparation of medicaments for the treatment of asthmatic airway remodelling in man.
机译:根据下式描述了一种使用肾上腺类固醇脱氢表雄酮及其某些类似物来减少永生和恶性细胞系生长的方法:根据以下化学式:其中X是卤素,羟基,氢,低级烷基或低级烷氧基; Y是氢或羟基; Z是低级烷基或氢。脱氢表雄酮及其有效类似物16 alpha -bromo-5-andtosten-17-one,16 beta -bromo-5-androsten-17-one,16 alpha -fluoro-5-androsten-17-one,16 beta -fluoro-5 -androsten-17-one,16 alpha -bromo-5-androstan-17-one,16 beta -bromo-5-androstan-17-one,16 alpha -fluoro-5-androstan-17-one和16 beta -fluoro -5-androstan-17-one损害了次级生长反应基因的激活,因此被证明可用于制备治疗人的哮喘气道重塑的药物。

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